QuickView for almotriptan (compound)

Summary
General Info

PubChem

PubChem Compound 123606

Name:	almotriptan
PubChem Compound ID:	123606
Molecular formula:	C₁₇H₂₅N₃O₂S
Molecular weight:	335.465 g/mol
Synonyms:	Almotriptan; KBio2_002408; Spectrum4_001134; Spectrum3_001006; Almotriptan (USAN); Spectrum2_000498; KBio3_001951; Spectrum_001884; D02824; KBio2_004976. show more » Almotriptan; KBio2_002408; Spectrum4_001134; Spectrum3_001006; Almotriptan (USAN); Spectrum2_000498; KBio3_001951; Spectrum_001884; D02824; KBio2_004976; SPBio_000395; KBio2_007544; PNU-180638; 154323-57-6; KBioGR_001647; Axert; KBioSS_002414; LAS-31416; Almogran show less «

DrugBank

Identification

Name:	almotriptan
Name (isomeric):	DB00918
Drug Type:	small molecule
Brand:	Almogran, Axert
Category:	Serotonin Agonists, Selective Serotonin Agonists, Vasoconstrictor Agents, Anti-migraine Agents, Anti-inflammatory Agents
CAS number:	181183-52-8

Pharmacology

Indication:	For the treatment of acute migraine headache in adults
Pharmacology:	Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamin... show more » Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT_1D family) having only a weak affinity for 5-HT_1A, 5-HT_5A, and 5-HT₇ receptors and no significant affinity or pharmacological activity at 5-HT₂, 5-HT₃ or 5-HT₄ receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT₁ receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans. show less «
Mechanism of Action:	Almotriptan binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction.
Protein binding:	35%
Route of elimination:	Almotriptan is eliminated primarily by renal excretion (about 75% of the oral dose), with approximately 40% of an administered dose excreted unchanged in urine. Approximately 13% of the administered dose is excreted via feces, both unchanged and metabolized.
Half Life:	3-4 hours
Clearance:	57 L/h [healthy] 34.2 L/h [moderate renal impairment (creatinine clearance between 31 and 71 mL/min)] 9.8 L/h [severe renal impairment (creatinine clearance between 10 and 30 mL/min)]
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

The absorption is unaffected by food.

Take without regard to meals.

Drug interaction:

Ergotamine	Possible severe and prolonged vasoconstriction
Fluvoxamine	Increased risk of CNS adverse effects
Tramadol	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Sibutramine	Increased risk of CNS adverse effects
Trimipramine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.

Ergotamine	Possible severe and prolonged vasoconstriction
Fluvoxamine	Increased risk of CNS adverse effects
Tramadol	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Sibutramine	Increased risk of CNS adverse effects
Trimipramine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Ketoconazole	This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
Nefazodone	Increased risk of CNS adverse effects
Escitalopram	Increased risk of CNS adverse effects
Dihydroergotoxine	Possible severe and prolonged vasoconstriction
Sertraline	Increased risk of CNS adverse effects
Ergonovine	Possible severe and prolonged vasoconstriction
Venlafaxine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Methysergide	Possible severe and prolonged vasoconstriction
Conivaptan	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Almotriptan. Use an initial almotriptan dose of 6.25mg when using almotriptan with a strong CYP3A4 inhibitor, and do not exceed 12.5mg of almotriptan in any 24-hour period. Avoid concurrent use of almotriptan with a strong CYP3A4 inhibitor in patients with impaired hepatic or renal function.
Citalopram	Increased risk of CNS adverse effects
Trazodone	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Desvenlafaxine	Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Voriconazole	Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of almotriptan by decreasing its metabolism. The initial and maximum doses should not exceed 6.25 mg and 12.5 mg, respectively during concomitant therapy. Concomitant therapy should be avoided in patients with impaired hepatic or renal function.
Paroxetine	Increased risk of CNS adverse effects
Isocarboxazid	The MAO inhibitor, isocarboxazid, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, almotriptan. Concomitant therapy is contraindicated.
Dihydroergotamine	Possible severe and prolonged vasoconstriction
Tranylcypromine	The MAO inhibitor, Tranylcypromine, may reduce the metabolism and clearance of the serotonin 5-HT1D receptor agonist, Almotriptan. Risk of serotonin syndrome and Almotriptan toxicity. Concomitant therapy should be avoided.
Methylergonovine	Possible severe and prolonged vasoconstriction
Phenelzine	The MAO inhibitor, phenelzine, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, almotriptan. Concomitant therapy is contraindicated.
Itraconazole	This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
Zolmitriptan	Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and almotriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
Fluoxetine	Increased risk of CNS adverse effects

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Targets

5-hydroxytryptamine 1B receptor

5-hydroxytryptamine 1D receptor

Enzymes

Amine oxidase [flavin-containing] A

Cytochrome P450 3A4

Cytochrome P450 2D6

Dimethylaniline monooxygenase [N-oxide-forming] 3